An efficient synthetic route to glycoamino acid building blocks for glycopeptide synthesis
An efficient synthetic route to glycoamino acid building blocks for glycopeptide synthesis
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DOI：
10.1021/ol048342n
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发表时间：
2004-10-28
期刊：
影响因子：
5.2
通讯作者：
Flitsch, SL
中科院分区：
文献类型：
--
作者：
Bejugam, M;Flitsch, SL
化学糖肽合成需要获得克量的糖基化氨基酸结构单元。因此，这种结构单元的合成效率是非常重要的。在这里，我们报告了一种快速，高效的合成路线，Fmoc保护的天冬酰胺糖苷从未保护的糖在三个步骤，高产率。通过标准Fmoc固相肽合成，将糖基化氨基酸成功掺入目标糖肽7和8中。
Chemical glycopeptide synthesis requires access to gram quantities of glycosylated amino acid building blocks. Hence, the efficiency of synthesis of such building blocks is of great importance. Here, we report a fast and highly efficient synthetic route to Fmoc-protected asparaginyl glycosides from unprotected sugars in three steps with high yields. The glycosylated amino acids were successfully incorporated into target glycopeptides 7 and 8 by standard Fmoc solid-phase peptide synthesis.